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1. 发明授权

US5668154A Pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles 失效
标题翻译：吡啶亚氨基-1,2-苯并异恶唑和 - 苯并异噻唑
公开(公告)号：US5668154A
公开(公告)日：1997-09-16
申请号：US637091
申请日：1996-05-02
申请人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
发明人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
IPC分类号： A61K31/44 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/28 , C07D231/56 , C07D261/20 , C07D275/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D401/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
摘要翻译：公开了新的吡啶亚甲基-1,2-苯并异恶唑和 - 苯并异噻唑，其制备方法和方法，以及利用1,2-苯并异恶唑和 - 苯并异噻唑及其中间体缓解记忆功能障碍和治疗抑郁症的方法或其组合物。

2. 发明授权

US5728717A Pyridiniminyl-1,2-benzisothiazoles 失效
标题翻译：吡啶亚甲基-1,2-苯并异噻唑
公开(公告)号：US5728717A
公开(公告)日：1998-03-17
申请号：US806981
申请日：1997-02-26
申请人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
发明人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
IPC分类号： A61K31/44 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/28 , C07D231/56 , C07D261/20 , C07D275/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D401/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
摘要翻译：公开了新的吡啶亚甲基-1,2-苯并异恶唑和 - 苯并异噻唑，其制备方法和方法，以及利用1,2-苯并异恶唑和 - 苯并异噻唑及其中间体缓解记忆功能障碍和治疗抑郁症的方法或其组合物。

3. 发明授权

US5948798A Pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles 失效
标题翻译：吡啶亚氨基-1,2-苯并异恶唑和 - 苯并异噻唑
公开(公告)号：US5948798A
公开(公告)日：1999-09-07
申请号：US961298
申请日：1997-10-30
申请人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
发明人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
IPC分类号： A61K31/44 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/28 , C07D231/56 , C07D261/20 , C07D275/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
摘要翻译：公开了新的吡啶亚甲基-1,2-苯并异恶唑和 - 苯并异噻唑，其制备方法和方法，以及利用1,2-苯并异恶唑和 - 苯并异噻唑及其中间体缓解记忆功能障碍和治疗抑郁症的方法或其组合物。

4. 发明授权

US6004977A N-(pyridinylamino) isoindolines and related compounds 失效
标题翻译： N-（吡啶基氨基）异吲哚啉和相关化合物
公开(公告)号：US6004977A
公开(公告)日：1999-12-21
申请号：US959789
申请日：1997-10-29
申请人： Barbara E. Kurys , David M. Fink , Brian S. Freed , Gregory H. Merriman
发明人： Barbara E. Kurys , David M. Fink , Brian S. Freed , Gregory H. Merriman
IPC分类号： C07D213/77 , C07D263/14 , C07D401/12 , C07D401/14 , A01N43/42 , A01N43/40 , C07C211/00 , C07D401/00
CPC分类号： C07D213/77 , C07D263/14 , C07D401/12 , C07D401/14
摘要： Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the N-(pyridinylamino)isoindolines and related compounds, the intermediates or compositions thereof are disclosed.
摘要翻译：公开了新型N-（吡啶基氨基）异吲哚啉及其制备方法，中间体及其制备方法，以及利用N-（吡啶基氨基）异吲哚啉及其相关化合物及其中间体或组合物缓解记忆功能障碍和治疗抑郁症的方法。

5. 发明授权

US5334599A Heteroaryl-8-azabicyclo[3,2,1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin 失效
标题翻译：杂芳基-8-氮杂双环[3,2,1]辛烷作为抗精神病药，5-HT3受体拮抗剂和5-羟色胺再摄取抑制剂
公开(公告)号：US5334599A
公开(公告)日：1994-08-02
申请号：US37134
申请日：1993-03-25
申请人： Edward J. Glamkowski , David M. Fink , Barbara E. Kurys , Yulin Chiang
发明人： Edward J. Glamkowski , David M. Fink , Barbara E. Kurys , Yulin Chiang
IPC分类号： C07D451/02 , C07D401/04 , A61K31/46 , C07D413/04 , C07D417/04
CPC分类号： C07D451/02
摘要： This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifiuoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifiuoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
摘要翻译：本发明涉及式（I）的化合物，其中X是-O - ， - S-或-NH-; Y是氢，卤素和低级烷氧基; p为1或2; n为2,3或4; R是氢，低级烷基，低级烷氧基，羟基，卤素，氨基，低级烷基氨基，硝基，低级烷硫基，三氟甲氧基，氰基，三氟甲基，R1是氢，低级烷基，低级烷氧基，卤素，羟基，羧基，低级烷基氨基，硝基，低级烷硫基，氰基和三氟甲基; m为1或2; 其药学上可接受的酸加成盐，以及适用的几何和旋光异构体及其外消旋混合物。本发明的化合物和组合物可用作5-HT 3受体拮抗剂的抗精神病药和5-羟色胺再摄取的抑制剂。

6. 发明授权

US5340936A 8-azabicyclo[3.2.1]octane methanone and corresponding oximes 失效
标题翻译： 8-氮杂双环[3.2.1]辛烷酮和相应的肟
公开(公告)号：US5340936A
公开(公告)日：1994-08-23
申请号：US37047
申请日：1993-03-25
申请人： Edward J. Glamkowski , David M. Fink , Barbara E. Kurys , Yulin Chiang
发明人： Edward J. Glamkowski , David M. Fink , Barbara E. Kurys , Yulin Chiang
IPC分类号： C07D451/02 , C07D401/04 , C07D417/04
CPC分类号： C07D451/02
摘要： This invention relates to compounds of the formula ##STR1## where X is --0--, --S--or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifiuoromethoxy, cyano, trifluoromethyl, ##STR2## where aryl is ##STR3## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifluoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic agent, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
摘要翻译：本发明涉及下式的化合物：其中X是-O - ， - S-或-NH-; Y是氢，卤素和低级烷氧基; p为1或2; n为2,3或4; R是氢，低级烷基，低级烷氧基，羟基，卤素，氨基，低级烷基氨基，硝基，低级烷硫基，三氟甲氧基，氰基，三氟甲基，其中芳基是氢，低级烷基，低级烷氧基，卤素，羟基，羧基，低级烷基氨基，硝基，低级烷硫基，氰基和三氟甲基; m为1或2; 其药学上可接受的酸加成盐，以及适用的几何和旋光异构体及其外消旋混合物。本发明的化合物和组合物可用作抗精神病药作为5-HT 3受体拮抗剂和作为5-羟色胺再摄取的抑制剂。

7. 发明授权

US5234931A Heteroaryl-8-azabicyclo[3.2.1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin 失效
标题翻译：杂芳基-8-氮杂双环[3.2.1]辛烷作为抗精神病药，5-HT3受体拮抗剂和5-羟色胺再摄取抑制剂
公开(公告)号：US5234931A
公开(公告)日：1993-08-10
申请号：US831027
申请日：1992-02-04
申请人： Edward J. Glamkowski , David M. Fink , Barbara E. Kurys , Yulin Chiang
发明人： Edward J. Glamkowski , David M. Fink , Barbara E. Kurys , Yulin Chiang
IPC分类号： C07D451/02
CPC分类号： C07D451/02
摘要： This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifluoromethoxy, cyano, trifluoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifluoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic agents, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
摘要翻译：本发明涉及式（I）的化合物，其中X是-O - ， - S-或-NH-; Y是氢，卤素和低级烷氧基; p为1或2; n为2,3或4; R是氢，低级烷基，低级烷氧基，羟基，卤素，氨基，低级烷基氨基，硝基，低级烷硫基，三氟甲氧基，氰基，三氟甲基，R 1是氢，低级烷基，低级烷氧基，卤素，羟基，羧基，低级烷基氨基，硝基，低级烷硫基，氰基和三氟甲基; m为1或2; 其药学上可接受的酸加成盐，以及适用的几何和旋光异构体及其外消旋混合物。本发明的化合物和组合物可用作抗精神病药作为5-HT 3受体拮抗剂和作为5-羟色胺再摄取的抑制剂。

8. 发明授权

US5726323A 4- and 6-carbamates related to physostigmine and intermediates for the preparation thereof 失效
标题翻译：与毒扁豆碱相关的4-和6-氨基甲酸酯及其制备的中间体
公开(公告)号：US5726323A
公开(公告)日：1998-03-10
申请号：US708590
申请日：1996-09-05
申请人： Edward J. Glamkowski , Barbara E. Kurys
发明人： Edward J. Glamkowski , Barbara E. Kurys
IPC分类号： C07D209/34 , C07D487/04
CPC分类号： C07D487/04 , C07D209/34
摘要： This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0, 1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.
摘要翻译：本发明涉及与式（I）的毒扁豆碱相关的4-和6-氨基甲酸酯，其中R1是烷基，环烷基，双环烷基，芳基或芳基低级烷基; R 2是氢或烷基，或者-NR 1 R 2一起形成5至12个碳的单环或双环; m为0,1或2; 每个X独立地是氢，卤素，低级烷基，硝基或氨基; 及其药学上可接受的酸加成盐，以及适用的几何和光学异构体及其外消旋混合物。本发明还涉及可用于制备4-和6-氨基甲酸酯的新型中间体。本发明的化合物显示用于减轻由胆碱能功能降低（诸如阿尔茨海默病）所特征的各种记忆功能障碍的效用。

9. 发明授权

US4983601A Benzo(b)pyrrolobenzodiazepines 失效
标题翻译：苯并（b）吡咯并苯并二氮杂卓
公开(公告)号：US4983601A
公开(公告)日：1991-01-08
申请号：US390130
申请日：1989-08-07
申请人： Edward J. Glamkowski , Barbara E. Kurys
发明人： Edward J. Glamkowski , Barbara E. Kurys
IPC分类号： C07D487/14 , A61K31/55 , A61P25/04 , C07D487/06 , C07D487/16
CPC分类号： C07D487/06
摘要： Novel benzo[b]pyrrolo[3,2,1-jk]benzodiazepines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing the compounds or compositions thereof are disclosed.

10. 发明授权

US5591864A 4-and 6-carbamates related to physostigmine and intermediates for the preparation thereof 失效
标题翻译：与毒扁豆碱相关的4-和6-氨基甲酸酯及其制备的中间体
公开(公告)号：US5591864A
公开(公告)日：1997-01-07
申请号：US873862
申请日：1992-04-27
申请人： Edward J. Glamkowski , Barbara E. Kurys
发明人： Edward J. Glamkowski , Barbara E. Kurys
IPC分类号： C07D209/34 , C07D487/04
CPC分类号： C07D487/04 , C07D209/34
摘要： This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0, 1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.
摘要翻译：本发明涉及与式（I）的毒扁豆碱相关的4-和6-氨基甲酸酯，其中R1是烷基，环烷基，双环烷基，芳基或芳基低级烷基; R 2是氢或烷基，或者-NR 1 R 2一起形成5至12个碳的单环或双环; m为0,1或2; 每个X独立地是氢，卤素，低级烷基，硝基或氨基; 及其药学上可接受的酸加成盐，以及适用的几何和光学异构体及其外消旋混合物。本发明还涉及可用于制备4-和6-氨基甲酸酯的新型中间体。本发明的化合物显示用于减轻由胆碱能功能降低（诸如阿尔茨海默病）所特征的各种记忆功能障碍的效用。

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